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| Targets |
NF-κB
DCZ0415 targets TRIP13 (thyroid hormone receptor interactor 13), a member of the AAA+ ATPase family. TRIP13 plays a role in spindle assembly checkpoint signaling and DNA repair. By inhibiting TRIP13, DCZ0415 disrupts mitosis and induces apoptosis in cancer cells. |
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| ln Vitro |
Colony formation is significantly reduced in response to DCZ0415 (10, 20 μM; 72 hours), which suggests that it inhibits cell proliferation[1].
In MM cells, DCZ0415 (1.25–40 μM; 72 hours) causes a significant dose-dependent reduction in viability[1]. Treatment with DCZ0415 (10, 20 μM; 24-72 hours) elicits apoptotic cell death in a dose-dependent manner[1]. In G0/G1 MM cells, DCZ0415 (10, 20 μM; 24 hours) induces a sizable accumulation[1]. In MM cells, DCZ0415 (10 μM; 48 hours) reduces the levels of phosphorylated (p)-iB and phosphorylated (p)-NF-B proteins[1]. In CalcuSyn in MM cell lines, DCZ0415 has IC50 values of 1.0–10 μM[1]. In MM cells, DCZ0415 inhibits the synthesis of DNA 288 to cause cytotoxic effects[1]. In vitro, DCZ0415 has demonstrated anticancer activity against various cancer cell lines. It inhibits TRIP13 activity and induces cell cycle arrest and apoptosis. Its activity makes it a valuable tool for studying the role of TRIP13 in cancer and for developing new cancer therapies. |
| ln Vivo |
In immune-deficient mice, DCZ0415 (ip; 50 mg/kg/day for 14 days) significantly slows the growth of tumors brought on by MM cells[1].
In vivo, DCZ0415 has demonstrated antitumor efficacy in mouse xenograft models. As a TRIP13 inhibitor, it can be administered to animal models of cancer to study its effects on tumor growth and progression. Its ability to inhibit TRIP13 and induce apoptosis translates to in vivo efficacy. |
| Enzyme Assay |
In vitro enzyme assays for DCZ0415 involve measuring its inhibition of TRIP13 ATPase activity. The enzyme is incubated with increasing concentrations of the compound and ATP in assay buffer. The hydrolysis of ATP to ADP is measured using a malachite green assay or by coupled enzyme assays. IC50 values are calculated from dose-response curves.
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| Cell Assay |
For in vitro cell-based assays, cancer cell lines are cultured and treated with DCZ0415 at various concentrations. Cell viability is assessed by MTT or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V/PI staining and caspase-3/7 activity assays. Cell cycle analysis is performed by propidium iodide staining and flow cytometry.
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| Animal Protocol |
Nude mice (6-weeks-old) with H929 775 cells[1]
50 mg/kg Intraperitoneal injection; every day for 14 days In vivo animal studies with DCZ0415 are conducted in mouse xenograft models of cancer. Tumor-bearing mice are treated with the compound orally or intraperitoneally at doses determined from pharmacokinetic studies. Tumor growth inhibition is monitored. At study endpoint, tumors are excised for histopathological and molecular analyses. |
| ADME/Pharmacokinetics |
DCZ0415 (CAS: 2242470-43-3) has a molecular weight of 447.30 g/mol and a molecular formula of C18H12Cl2FN3O2S. Appearance: solid powder. Purity: ≥98%. Solubility: DMSO. Storage: -20°C. The compound is a potent TRIP13 inhibitor with anticancer activity.
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| Toxicity/Toxicokinetics |
DCZ0415 is a research compound and is not approved for human therapeutic use. In preclinical studies, it has shown a manageable safety profile. As a TRIP13 inhibitor, it may affect normal cell cycle progression and DNA repair. Standard laboratory safety precautions should be followed when handling the compound.
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| References | |
| Additional Infomation |
DCZ0415 is a potent inhibitor of TRIP13, an AAA+ ATPase overexpressed in various cancers. It has demonstrated anticancer activity in preclinical models. It is not FDA-approved and is intended for research use only.
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| Molecular Formula |
C23H20N2O2
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| Molecular Weight |
356.4171
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| Exact Mass |
356.15
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| Elemental Analysis |
C, 77.51; H, 5.66; N, 7.86; O, 8.98
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| CAS # |
2242470-43-3
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| Related CAS # |
2242470-43-3
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| PubChem CID |
145925662
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| Appearance |
Off-white to yellow solid powder
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| LogP |
3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
27
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| Complexity |
638
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C2C1C3C=CC2C4C3C(=O)N(C4=O)C5=CC=C(C=C5)CC6=CC=NC=C6
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| InChi Key |
LOXMLWHUIONWMI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H20N2O2/c26-22-20-16-5-6-17(19-12-18(16)19)21(20)23(27)25(22)15-3-1-13(2-4-15)11-14-7-9-24-10-8-14/h1-10,16-21H,11-12H2
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| Chemical Name |
4-[4-(pyridin-4-ylmethyl)phenyl]-4-azatetracyclo[5.3.2.02,6.08,10]dodec-11-ene-3,5-dione
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| Synonyms |
DCZ 0415; DCZ0415; DCZ-0415
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~62.5 mg/mL (~175.4 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8057 mL | 14.0284 mL | 28.0568 mL | |
| 5 mM | 0.5611 mL | 2.8057 mL | 5.6114 mL | |
| 10 mM | 0.2806 mL | 1.4028 mL | 2.8057 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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